rheum week 4

What are the different classes of opioid analgesics?

Opioid analgesics include natural opioids, semi-synthetic opioids, and synthetic opioids.

What is the mechanism of action of opioid analgesics?

Opioid analgesics work by binding to opioid receptors in the brain and spinal cord, inhibiting pain signal transmission.

What are the different opioid receptors and their effects?

The main opioid receptors are mu, delta, and kappa, each producing varying effects such as analgesia, euphoria, and sedation.

How do the metabolism processes of opioid analgesics differ?

Opioids are metabolized primarily in the liver, with variations in half-life and active metabolites affecting their duration and potency.

What factors influence the potency of opioid analgesics?

Potency is influenced by receptor affinity, dose, and individual patient factors such as genetics and tolerance.

What are opioids with both opioid and non-opioid effects?

Some opioids, like tramadol, have additional mechanisms that include serotonin and norepinephrine reuptake inhibition.

What is meant by tolerance in opioid use?

Tolerance refers to a reduced response to a drug after repeated use, requiring higher doses to achieve the same effect.

What is physical dependence in the context of opioids?

Physical dependence occurs when the body adapts to a drug, leading to withdrawal symptoms if the drug is abruptly discontinued.

What are opioid antagonists?

Opioid antagonists, such as naloxone, block the effects of opioids and are used to reverse opioid overdoses.

What is opioid-induced hyperalgesia?

Opioid-induced hyperalgesia is a condition where prolonged opioid use leads to increased sensitivity to pain.

What types of antidepressants are used as adjuvant analgesics?

Tricyclic antidepressants and SNRIs are commonly used as adjuvant analgesics for chronic pain management.

How are anticonvulsants used as adjuvant analgesics?

Anticonvulsants, such as gabapentin and pregabalin, are used to treat neuropathic pain by stabilizing nerve activity.

What role do NMDA receptor antagonists play in analgesia?

NMDA receptor antagonists, like ketamine, can reduce pain by blocking excitatory neurotransmission in the central nervous system.

How are local anesthetics used as adjuvant analgesics?

Local anesthetics provide pain relief by blocking nerve conduction in a specific area, often used in conjunction with other analgesics.

What are topical adjuvant analgesics?

Topical adjuvant analgesics include agents like lidocaine patches and capsaicin cream, applied directly to the skin to relieve localized pain.

What other agents may be used as adjuvant analgesics?

Agents such as alpha-2 agonists, corticosteroids, and muscle relaxants can also be utilized to enhance pain management.

What is the action of cannabinoids like THC and CBD on the endocannabinoid system?

Cannabinoids interact with the endocannabinoid system and other receptors to modulate pain, inflammation, and mood.

What are the key cannabinoid concentrations for managing medical conditions?

Different cannabinoid concentrations are appropriate for various medical conditions.

What is the pharmacokinetic activity of medicinal cannabis?

It involves the absorption, distribution, metabolism, and excretion of cannabinoids.

What are the common dosage forms of medicinal cannabis?

Dosage forms include oils, capsules, edibles, and inhalants.

What evidence supports the use of medicinal cannabis in pain management?

Clinical studies indicate its effectiveness in reducing chronic pain.

What safety considerations are important for medicinal cannabis use?

Considerations include potential drug interactions and side effects.

What are the dosing recommendations for medicinal cannabis?

Dosing should be individualized based on patient response and condition.

What regulatory aspects govern medicinal cannabis supply?

Pharmacists must comply with Federal and State regulations regarding cannabis.

What important counselling points should pharmacists provide for medicinal cannabis?

Pharmacists should inform patients about dosing, side effects, and interactions.

What are opioids?

Natural peptides synthesized as large inactive precursors that modulate pain and other systems.

What are the main receptors for opioids?

Mu, delta, kappa, and orl-1 receptors.

What is the primary mechanism of action (MOA) of opioids?

Opioids reduce calcium influx and inhibit neurotransmitter release.

What are some non-analgesic effects of opioids?

Effects include nausea, respiratory depression, and urinary retention.

What is tolerance in the context of opioid use?

Tolerance is when increased doses are required to achieve the same effect.

What is opioid dependence?

A state where withdrawal symptoms occur upon cessation of opioids.

What are the classifications of opioids?

Natural (e.g., morphine), semi-synthetic (e.g., oxycodone), and synthetic (e.g., fentanyl).

What is the potency of codeine compared to morphine?

Codeine is approximately 1/10th as potent as morphine.

What are the side effects of tramadol?

Seizures and serotonin toxicity can occur, especially with drug interactions.

What is the significance of morphine's glucuronidation?

It converts morphine to M6G (active) and M3G (inactive), affecting analgesic potency.

What is the role of naloxone?

Naloxone is used to reverse opioid-induced respiratory depression and overdose.

What is the purpose of methylnaltrexone?

It is used for acute relief of severe opioid-induced constipation.

What are the safety factors when prescribing opioids?

Doses should be 25-50% lower than the equal dose range and titrated according to response.

What are the monitoring parameters for opioid therapy?

Monitor activity, analgesia, adverse effects, aberrant behavior, and affect.

What is the mechanism of action of NSAIDs?

NSAIDs inhibit prostaglandin synthesis, increasing pain threshold and reducing inflammation.

What are the risks associated with NSAIDs?

Major gastrointestinal and renal adverse effects, including potential for nephritis.

What is the difference between COX-1 and COX-2?

COX-1 is involved in gastric protection, while COX-2 is associated with inflammation and pain.

What is the effect of aspirin on platelets?

Aspirin irreversibly inhibits COX, leading to prolonged antiplatelet effects.

What is the 'triple whammy' in renal safety?

The combination of NSAIDs, diuretics, and ACE/ARBs increases renal side effects.

What effect does competitive inhibition of the acetylation site of COX have on aspirin?

It decreases aspirin's anti-platelet effects.

Which medications should be avoided in combination with aspirin?

Celecoxib, naproxen, and indomethacin.

What is the first-line antidepressant for chronic pain management?

Amitriptyline and nortriptyline (TCA).

What is the order of effectiveness for antidepressants in chronic pain?

TCA > SNRI > SSRI.

What type of pain is best treated with noradrenergic TCAs?

Neuropathic pain.

What is the role of anticonvulsants in pain management?

They reduce excitability of damaged neurons and treat neuropathic pain.

What are gabapentinoids and how do they function?

Gabapentin and pregabalin block calcium channels to reduce neurotransmitter release.

What is the primary use of local anesthetics in pain management?

To interrupt transmission of nociceptive information from the PNS to the brain.

What is the mechanism of NMDA antagonists in pain management?

They inhibit glutamate activation, which increases pain response.

What are the adverse effects of SNRIs?

They may aggravate hypertension, seizures, and trigger mania.

What is the significance of ketamine in pain management?

It acts as an NMDA receptor antagonist and has analgesic effects at certain plasma levels.

What is the primary use of topical adjuvant analgesics like lidocaine?

To provide localized pain relief, especially in postherpetic neuralgia.

What is the role of capsaicin in pain management?

It desensitizes TRPV1 receptors to treat osteoarthritis and neuropathic pain.

What is the function of alpha-2 agonists like clonidine in pain management?

They reduce neurogenic pain in patients with cancer pain responding to opioids.

What is the role of bisphosphonates in cancer-related pain?

They prevent and treat skeletal complications of bone metastases.

What are the common side effects of skeletal muscle relaxants?

Sedation, dizziness, and potential dependence.

What type of pain do smooth muscle relaxants target?

Visceral distention pain and colic.

What is the recommended treatment for trigeminal neuralgia?

Carbamazepine is the first-line treatment.

What is the mechanism of action for gabapentin?

It blocks N, P, Q type calcium channels to reduce pain signaling.

What is the benefit of using pregabalin for neuropathic pain?

It is effective for diverse types of neuropathic pain and has prolonged benefits.

What is the significance of gradual withdrawal from antidepressants?

To prevent withdrawal reactions that may occur with abrupt cessation.

What is the primary action of tricyclic antidepressants (TCAs)?

They act as noradrenergic agents to alleviate chronic pain.

What are the side effects of using topical lidocaine patches?

Low adverse effects, but may cause local irritation.

What is the role of steroids in pain management?

They can help with nerve root/trunk compression and spinal cord compression.

What is the mechanism of action of valproate in pain management?

It has multimodal action beneficial in cancer-related pain.

What are the primary active components of cannabis?

THC (tetrahydrocannabinol) and CBD (cannabidiol)

What is the primary psychoactive component of cannabis?

THC

What is CBD known for?

Non-intoxicating properties that alleviate symptoms of psychosis and anxiety.

What is the endocannabinoid system?

A neuromodulatory system in the body that includes endogenous cannabinoids, receptors, and enzymes.

What are endocannabinoids?

Cannabinoids created by the body that exert actions at receptors.

What are the two most abundant endocannabinoids?

Anandamide (AEA) and 2-arachidonoyl glycerol ether (2-AG).

Where are CB1 receptors primarily found?

In the brain and spinal cord.

What effects does THC have when activating CB1 receptors?

It modulates neurotransmitters, influencing pain, appetite, and cognition.

What is the pharmacodynamic action of THC?

Produces euphoria, relaxation, increases appetite, and has analgesic properties.

What therapeutic properties does CBD exhibit?

Anti-inflammatory, immunomodulatory, antioxidant, and neuroprotective properties.

What are chemovars in cannabis?

Different strains of cannabis that vary in concentrations of CBD and THC.

What is the significance of terpenes in cannabis?

Organic compounds that provide protection and attract pollinators, with potential therapeutic effects.

How is THC absorbed when cannabis is inhaled?

Rapidly from the lungs, reaching the brain within 1-3 minutes.

What is the duration of effects from inhaled cannabis?

2-4 hours.

What is the absorption profile of oral cannabis?

Slower absorption (30-90 minutes) with effects lasting 8-24 hours.

What is SAS Cat A in relation to cannabis access?

Allows access to cannabis for seriously ill patients without usual quality and safety data requirements.

What is SAS Cat B?

Main pathway for cannabis access requiring thorough clinical justification for use.

What are common adverse effects of cannabis?

Drowsiness, dizziness, dry mouth, anxiety, and cognitive impairment.

What factors increase the risk of psychosis with cannabis use?

Younger age, high-dose long-term use, and family history of schizophrenia.

What is the recommended approach for dosing cannabis?

Highly individualized; start low and go slow.

What is the role of the TGA in cannabis prescription?

Responsible for providing access to unapproved cannabis products.

What is the significance of the 1:1 ratio in medicinal cannabis?

It may improve overall tolerability and effectiveness of the extract.

What are the potential drug interactions with cannabis?

Concurrent use with other CNS depressants and drugs metabolized by the CYP450 system.

What should be considered before prescribing cannabis?

Comprehensive clinical assessment, including past medical history and risk factors.

What is the evidence quality for therapeutic uses of cannabis?

Typically moderate to low, with few studies comparing effects against approved treatments.

What is the effect of CBD on THC's psychoactive effects?

CBD may reduce or modulate some psychoactive effects of THC.

What is the significance of cannabinoid ratios in medicinal products?

They determine the pharmacological effects and therapeutic outcomes.

What is the role of pharmacists in cannabis dispensing?

Ensure prescriptions meet requirements and manage patient counseling.

What is the legal status of cannabis in Australia as of November 2016?

Legislation was passed allowing cultivation, prescribing, and dispensing for medicinal purposes.